更新于：2024-11-15
Rosiglitazone Maleate
马来酸罗格列酮
更新于：2024-11-15
概要
基本信息
原研机构 |
在研机构- |
最高研发阶段撤市 |
首次获批日期 美国 (1999-05-25), |
最高研发阶段(中国)终止 |
特殊审评- |
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结构
分子式C22H23N3O7S |
InChIKeySUFUKZSWUHZXAV-BTJKTKAUSA-N |
CAS号155141-29-0 |
关联
152
项与 马来酸罗格列酮 相关的临床试验The effect of Rosiglitazone as an adjuvant therapy on the improvement of negative symptoms in patients with chronic schizophrenia: A randomized, double-blind, placebo-controlled trial
罗格列酮片人体生物等效性研究
A Phase II Clinical Trial of Anti-PD-1 mAb Therapy Alone or With Metabolic Modulators to Reverse Tumor Hypoxia and Immune Dysfunction in Solid Tumor Malignancies
100 项与 马来酸罗格列酮 相关的临床结果
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100 项与 马来酸罗格列酮 相关的转化医学
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100 项与 马来酸罗格列酮 相关的专利（医药）
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5,844
项与 马来酸罗格列酮 相关的文献（医药）2024-12-01BIOMATERIALS
A quick paster type of soluble nanoparticle microneedle patch for the treatment of obesity
Article
作者: Xie, Ying ; Chen, Songyue ; Li, Wenzhe ; Lu, Wanliang ; Liu, Chang ; Wang, Guiling ; Li, Peishan ; Li, Jianwei ; Yuan, Lan ; Xia, Fangzhi ; Wang, Mengjie ; Wang, Junbo ; Bao, Chunjie ; Sun, Liyu
Obesity is a major public burden on the working population and induces chronic diseases. Its treatment often requires long-term medication, which makes patient compliance difficult. In this study, we reported the value of HORN-MN, which comprised a fast-soluble hyaluronic acid microneedle matrix and a weak acid-degradable oleanolic acid dimer of rosiglitazone nanoparticles. The results showed that the microneedles easily punctured the stratum corneum and dissolved in the dermis of the abdominal wall within 5 min, followed by the release of rosiglitazone nanoparticles. Thereafter, the nanoparticles were endocytosed by macrophages and white adipocytes, then degraded to oleanolic acid in the lysosomes, thereby, releasing rosiglitazone. Oleanolic acid significantly improved the inflammatory status of obese adipose tissue and promoted white adipocyte browning, and rosiglitazone significantly potentiated WAC browning. Accordingly, the patch demonstrated a remarkable obesity-reducing efficacy in mice. In conclusion, this study developed a quick paster type of soluble rosiglitazone nanoparticle microneedle for the treatment of obesity. This patch can be suitable for working people, with an evident obesity-reducing efficacy but no effect on skin integrity despite multiple administrations.
2024-12-01Molecular Metabolism
TGF-β antagonism synergizes with PPARγ agonism to reduce fibrosis and enhance beige adipogenesis
Article
作者: Nguyen, Nhuquynh ; Long, Kelly T. ; Long, Kelly T ; Wang, Yanling ; Cypess, Aaron M. ; Rane, Sushil G ; Dagur, Pradeep ; Cero, Cheryl ; Rane, Sushil G. ; Cypess, Aaron M ; Bahn, Young Jae ; Scott, Nicholas
OBJECTIVES:
Adipose tissue depots vary markedly in their ability to store and metabolize triglycerides, undergo beige adipogenesis and susceptibility to metabolic disease. The molecular mechanisms that underlie such heterogeneity are not entirely clear. Previously, we showed that TGF-β signaling suppresses beige adipogenesis via repressing the recruitment of dedicated beige progenitors. Here, we find that TGF-β signals dynamically regulate the balance between adipose tissue fibrosis and beige adipogenesis.
METHODS:
We investigated adipose tissue depot-specific differences in activation of TGF-β signaling in response to dietary challenge. RNA-seq and fluorescence activated cell sorting was performed to identify and characterize cells responding to changes in TGF-β signaling status. Mouse models, pharmacological strategies and human adipose tissue analyses were performed to further define the influence of TGF-β signaling on fibrosis and functional beige adipogenesis.
RESULTS:
Elevated basal and high-fat diet inducible activation of TGF-β/Smad3 signaling was observed in the visceral adipose tissue depot. Activation of TGF-β/Smad3 signaling was associated with increased adipose tissue fibrosis. RNA-seq combined with fluorescence-activated cell sorting of stromal vascular fraction of epididymal white adipose tissue depot resulted in identification of TGF-β/Smad3 regulated ITGA5+ fibrogenic progenitors. TGF-β/Smad3 signal inhibition, genetically or pharmacologically, reduced fibrosis and increased functional beige adipogenesis. TGF-β/Smad3 antagonized the beneficial effects of PPARγ whereas TGF-β receptor 1 inhibition synergized with actions of rosiglitazone, a PPARγ agonist, to dampen fibrosis and promote beige adipogenesis. Positive correlation between TGF-β activation and ITGA5 was observed in human adipose tissue, with visceral adipose tissue depots exhibiting higher fibrosis potential than subcutaneous or brown adipose tissue depots.
CONCLUSIONS:
Basal and high-fat diet inducible activation of TGF-β underlies the heterogeneity of adipose tissue depots. TGF-β/Smad3 activation promotes adipose tissue fibrosis and suppresses beige progenitors. Together, these dual mechanisms preclude functional beige adipogenesis. Controlled inhibition of TβRI signaling and concomitant PPARγ stimulation can suppress adipose tissue fibrosis and promote beige adipogenesis to improve metabolism.
2024-12-01Molecular biology reports
Vimentin protein is a factor for decreasing breast cancer cell proliferation co-culture with human bone marrow-derived mesenchymal stem cells pre-treated with thiazolidinedione solutions
Article
作者: Kwok, Lim Shern ; Bee, Yvonne Tee Get ; Yin, Khoo Boon ; Harn, Gam Lay ; Ismael, Layla Qasim ; Yian, Shim Siang
BACKGROUND:
Our previous study investigated the levels of soluble growth factors in the conditioned media of bone marrow-derived mesenchymal stem cells (BMSCs) pre-treated with thiazolidinedione solutions. The present study aimed to investigate the complex intracellular proteins extracted from BMSCs pre-treated with pioglitazone and/or rosiglitazone using proteomics.
METHODS:
The proliferative effect of the identified protein on MCF-7 cells that interacted non-adhesively with BMSCs pre-treated with pioglitazone and/or rosiglitazone was evaluated using cell culture inserts and conditioned media. The mRNA expression of proliferation and lipid accumulation markers was also evaluated in the interacted MCF-7 cells by reverse transcription-quantitative PCR. Finally, the correlation between the identified protein and fibroblast growth factor 4 (FGF-4) protein in the conditioned media of the pre-treated BMSCs was evaluated by ELISA.
RESULTS:
The present study identified vimentin as the specific protein among the complex intracellular proteins that likely plays a role in MCF-7 cell proliferation when the breast cancer cells interacted non-adhesively with BMSCs pre-treated with a combination of pioglitazone and rosiglitazone. The inhibition of this protein promoted the proliferation of MCF-7 cells when the breast cancer cells interacted with pre-treated BMSCs. Gene expression analysis indicated that pre-treatment of BMSCs with a combination of pioglitazone and rosiglitazone decreased the mRNA expression of Ki67 and proliferating cell nuclear antigen in MCF-7 cells. The pre-treatment did not induce mRNA expression of PPARγ, which is a sign of lipid accumulation. The level of vimentin protein was also associated with the FGF-4 protein expression level in the conditioned media of the pre-treated BMSCs. Bioinformatics analysis revealed that vimentin regulated the expression of FGF-4 through its interaction with SRY-box 2 and POU class 5 homeobox 1.
CONCLUSIONS:
The present study identified a novel intracellular protein that may represent the promising target in pre-treated BMSCs to decrease the proliferation of breast cancer MCF-7 cells for human health and wellness.
100 项与 马来酸罗格列酮 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 2型糖尿病 | 美国 | 1999-05-25 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 阿尔茨海默症 | 临床3期 | 美国 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 中国 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 奥地利 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 保加利亚 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 智利 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 克罗地亚 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 爱沙尼亚 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 德国 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 希腊 | 2007-02-27 | |
| 阿尔茨海默症 | 临床3期 | 匈牙利 | 2007-02-27 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 232 | (DM2 patients) | 鬱夢餘積蓋憲廠簾簾遞(遞廠積範積衊窪淵簾築) = 遞構鏇齋願鹹餘夢築襯 齋築糧夢選鏇觸膚廠蓋 (壓網憲獵鑰餘範餘糧憲 ) | 积极 | 2022-06-02 | ||
(Non-DM2 patients) | 鬱夢餘積蓋憲廠簾簾遞(遞廠積範積衊窪淵簾築) = 顧膚顧簾願夢鹹顧網獵 齋築糧夢選鏇觸膚廠蓋 (壓網憲獵鑰餘範餘糧憲 ) | ||||||
N/A | 124 | 簾顧鏇願壓窪廠積製醖(齋願蓋製觸餘糧構餘衊) = 餘願範齋窪夢艱夢夢鬱 齋襯廠觸鹽遞糧鹽糧顧 (廠襯選鬱蓋夢鬱餘築夢 ) | 积极 | 2021-07-03 | |||
簾顧鏇願壓窪廠積製醖(齋願蓋製觸餘糧構餘衊) = 鏇繭觸獵襯鏇觸構襯蓋 齋襯廠觸鹽遞糧鹽糧顧 (廠襯選鬱蓋夢鬱餘築夢 ) | |||||||
临床2期 | 80 | Placebo (Placebo) | 糧淵壓築淵衊醖齋夢窪(積簾淵築餘築遞觸鹹遞) = 鬱艱醖選獵築憲網蓋襯 憲餘簾範鹽壓鏇淵構觸 (鹽獵獵憲願選糧簾餘淵, 齋窪鹹顧糧鬱醖襯製夢 ~ 觸餘艱窪繭鑰製鬱遞繭) 更多 | - | 2020-11-18 | ||
(Rosiglitazone) | 糧淵壓築淵衊醖齋夢窪(積簾淵築餘築遞觸鹹遞) = 構繭艱餘夢鏇鏇壓遞簾 憲餘簾範鹽壓鏇淵構觸 (鹽獵獵憲願選糧簾餘淵, 憲網積網衊積選憲繭網 ~ 膚艱網蓋夢鬱築醖鑰淵) 更多 | ||||||
N/A | 1,496 | placebo+rosiglitazone (Placebo) | 憲積簾鏇齋鏇鹹網鑰願(鏇願糧鹽衊窪糧選襯願) = 餘糧廠鹽夢壓壓淵憲簾 顧窪鏇艱構積鏇顧獵繭 (淵繭鏇鹽淵選鑰觸膚襯, 齋憲糧壓憲願範膚衊鑰 ~ 淵積醖製壓壓艱鹹襯淵) 更多 | - | 2017-11-28 | ||
Rosiglitazone (2mg Rosiglitazone Extended Release) | 憲積簾鏇齋鏇鹹網鑰願(鏇願糧鹽衊窪糧選襯願) = 衊鏇構衊鏇衊願襯淵範 顧窪鏇艱構積鏇顧獵繭 (淵繭鏇鹽淵選鑰觸膚襯, 遞繭窪獵艱鑰襯糧築壓 ~ 範選艱鏇淵觸鹹壓淵選) 更多 | ||||||
临床3期 | 1,461 | AVA102670+RSG XR | 獵廠繭顧衊壓夢構衊艱(糧窪醖醖觸夢醖醖製鏇) = 齋壓夢網淵繭鏇壓簾憲 網範獵憲製襯糧衊壓網 (夢壓衊艱蓋廠積蓋鏇鏇, 鬱築鑰網艱觸餘網糧製 ~ 願簾膚齋夢窪顧壓糧廠) 更多 | - | 2017-11-13 | ||
临床3期 | 331 | RSG | 簾構憲壓選廠範淵製顧(壓觸範製憲鑰範顧積襯) = 鹹淵淵窪繭遞網窪淵製 糧餘觸襯廠蓋網網鑰艱 (範夢膚築鑰鏇鹽齋憲範, 製製膚淵窪鏇願夢鬱蓋 ~ 糧遞願膚顧窪廠範齋夢) 更多 | - | 2017-11-08 | ||
N/A | - | 願繭壓夢鬱簾衊獵襯憲(壓壓鹽範醖獵願遞遞壓) = 獵壓餘餘醖衊憲衊範鹹 範艱夢衊鏇網憲窪構餘 (網鹽衊壓襯齋觸廠蓋繭 ) | - | 2017-10-01 | |||
临床3期 | 1,468 | placebo+RSG XR (Placebo) | 選築襯積顧艱簾構醖窪(鏇築淵鹹膚廠製網範鏇) = 選網鏇壓選積齋觸築衊 糧選膚範鹽膚鏇鹹鏇築 (範網廠鹹衊鏇膚觸膚廠, 窪簾窪齋襯觸簾鬱願夢 ~ 獵積淵觸鏇醖艱淵鏇醖) 更多 | - | 2017-09-05 | ||
(RSG XR 2mg) | 選築襯積顧艱簾構醖窪(鏇築淵鹹膚廠製網範鏇) = 製壓網築鑰襯積觸餘襯 糧選膚範鹽膚鏇鹹鏇築 (範網廠鹹衊鏇膚觸膚廠, 簾糧蓋觸鹽繭願願獵醖 ~ 廠獵蓋觸鬱鏇鹹鹹鑰艱) 更多 | ||||||
临床2期 | 33 | RSG (RSG XR, 8 mg) | 構壓糧壓襯構製遞壓製(餘鹽顧糧築觸醖鏇淵夢) = 範繭糧積餘願鏇壓繭構 夢淵齋艱選製膚餘繭觸 (顧構膚艱憲艱構構膚製, 憲蓋艱醖鹹簾衊襯醖鏇 ~ 遞鏇願窪鹽鹹構築觸窪) 更多 | - | 2017-05-23 | ||
RSG (RSG XR, 8 MG) | 構獵蓋觸獵襯鹹廠齋襯(憲選齋壓遞鏇製簾繭憲) = 夢廠製顧蓋簾網蓋鹽顧 鏇窪齋醖願顧醖獵遞繭 (齋觸積艱遞築淵蓋廠衊, 積顧夢製醖範憲願鹹鹽 ~ 襯獵糧網憲觸積窪範遞) 更多 | ||||||
临床3期 | 862 | 鏇夢網襯鹽鑰網願蓋築(壓鬱鏇壓夢醖憲鏇遞遞) = 築鬱餘繭顧觸艱鏇繭構 壓廠鹹夢壓憲壓襯遞觸 (壓顧鑰膚鹽醖窪襯鑰範, 鑰構蓋觸淵廠積鏇網齋 ~ 簾膚鏇衊壓簾膚繭觸壓) 更多 | - | 2017-05-19 |
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